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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共19条记录   Charting, Navigating, and Populating Natural Product Chemical Space for Drug Discovery [作者：LACHANCE HUGO; WETZEL STEFAN; KUMAR KAMAL; WALDMANN HERBERT,期刊：Journal of Medicinal Chemistry, 页码：5989-6001 , 文章类型： Article，,卷期：2012年55-13] Mitigating Heterocycle Metabolism in Drug Discovery [作者：ST JEAN DAVID J JR; FOTSCH CHRISTOPHER,期刊：Journal of Medicinal Chemistry, 页码：6002-6020 , 文章类型： Article，,卷期：2012年55-13] A Peptide Nucleic Acid-Aminosugar Conjugate Targeting Transactivation Response Element of HIV-1 RNA Genome Shows a High Bioavailability in Human Cells and Strongly Inhibits Tat-Mediated Transactivation of HIV-1 Transcription [作者：DAS INDRAJIT; DESIRE JEROME; MANVAR DINESH; BAUSSANNE ISABELLE; PANDEY VIRENDRA N; DECOUT JEANLUC,期刊：Journal of Medicinal Chemistry, 页码：6021-6032 , 文章类型： Article，,卷期：2012年55-13] The 6-aminoglucosamine ring of the aminoglycoside antibiotic neomycin B (ring II) was conjugated to a 16-mer peptide nucleic acid (PNA) targeting HIV-I TAR RNA. For this purpose, we prepared the aminoglucosamine monomer ... Design, Synthesis, and Preliminary Biological Evaluation of 6-O-Glucose-Azomycin Adducts for Diagnosis and Therapy of Hypoxic Tumors [作者：KUMAR PIYUSH; SHUSTOV GENNADY; LIANG HONG; KHLEBNIKOV VLADIMIR; ZHENG WEIZHONG; YANG XIAOHONG; CHEESEMAN CHRIS; WIEBE LEONARD I,期刊：Journal of Medicinal Chemistry, 页码：6033-6046 , 文章类型： Article，,卷期：2012年55-13] Several 2-nitroimidazole-based molecules (NIs) are used as clinical hypoxic tumor radiodiagnostics, but they are not effective as radiosensitizers/radiochemotherapeutics. These NIs permeate tumor cells nonselectively via... Discovery and Optimization of Benzotriazine Di-N-Oxides Targeting Replicating and Nonreplicating Mycobacterium tuberculosis [作者：CHOPRA SIDHARTH; KOOLPE GARY A; TAMBOONG ARLYN A; MATSUYAMA KAREN N; RYAN KENNETH J; TRAN TRAN B; DOPPALAPUDI RUPA S; RICCIO EDWARD S; IYER LALITHA V; GREEN CAROL E; WAN BAOJIE; FRANZBLAU SCOTT G; MADRID PETER B,期刊：Journal of Medicinal Chemistry, 页码：6047-6060 , 文章类型： Article，,卷期：2012年55-13] Compounds bactericidal against both replicating and nonreplicating Mtb may shorten the length of TB treatment regimens by eliminating infections more rapidly. Screening of a panel of antimicrobial and anticancer drug cla... Design, Synthesis, and Biological Evaluation of N-Alkylated Deoxynojirimycin (DNJ) Derivatives for the Treatment of Dengue Virus Infection [作者：YU WENQUAN; GILL TINA; WANG LIJUAN; DU YANMING; YE HONG; QU XIAOWANG; GUO JUTAO; CUCONATI ANDREA; ZHAO KANG; BLOCK TIMOTHY M; XU XIAODONG; CHANG JINHONG,期刊：Journal of Medicinal Chemistry, 页码：6061-6075 , 文章类型： Article，,卷期：2012年55-13] We recently described the discovery of oxygenated N-alkyl deoxynojirimycin (DNJ) derivative 7 (CM-10-18) with antiviral activity against dengue virus (DENY) infection both in vitro and in vivo. This imino sugar was promi... Anticancer Activity and Cellular Repression of c-MYC by the G-Quadruplex-Stabilizing 11-Piperazinylquindoline Is Not Dependent on Direct Targeting of the G-Quadruplex in the c-MYC Promoter [作者：BODDUPALLY PEDA V L; HAHN SEONGMIN; BEMAN CRISTINA; DE BISWANATH; BROOKS TRACY A; GOKHALE VIJAY; HURLEY LAURENCE H,期刊：Journal of Medicinal Chemistry, 页码：6076-6086 , 文章类型： Article，,卷期：2012年55-13] This G-rich region of the c-MYC promoter has been shown to form a G-quadruplex structure that acts as a silencer element for c-MYC transcriptional control. In the present work, we have synthesized a series of 11-substitu... Lead Optimization of Antimalarial Propafenone Analogues [作者：LOWES DAVID; PRADHAN ANUPAM; IYER LALITHA V; PARMAN TOUFAN; GOW JASON; ZHU FANGYI; FURIMSKY ANNA; LEMOFF ANDREW; GUIGUEMDE W ARMAND; SIGAL MARTINA; CLARK JULIE A; WILSON EMILY; TANG LIANG; CONNELLY MICHELE C; DERISI JOSEPH L; KYLE DENNIS E; MIRSALIS JON; GUY R KIPLIN,期刊：Journal of Medicinal Chemistry, 页码：6087-6093 , 文章类型： Article，,卷期：2012年55-13] Previously reported studies identified analogues of propafenone that had potent antimalarial activity, reduced cardiac ion channel activity, and properties that suggested the potential for clinical development for malari... Ligand Binding Stepwise Disrupts Water Network in Thrombin: Enthalpic and Entropic Changes Reveal Classical Hydrophobic Effect [作者：BIELA ADAM; SIELAFF FRANK; TERWESTEN FELIX; HEINE ANDREAS; STEINMETZER TORSTEN; KLEBE GERHARD,期刊：Journal of Medicinal Chemistry, 页码：6094-6110 , 文章类型： Article，,卷期：2012年55-13] Well-ordered water molecules are displaced from thrombin's hydrophobic S3/4-pocket by P3-varied ligands (Gly, D-Ala, D-Val, D-Leu to D-Cha with increased hydrophobicity and steric requirement). Two series with 2-(aminome... N '-Substituted-2 '-O,3 '-N-carbonimidoyl Bridged Macrolides: Novel Anti-inflammatory Macrolides without Antimicrobial Activity [作者：BOSNAR MARTINA; KRAGOL GORAN; KOSTRUN SANJA; VUJASINOVIC INES; BOSNJAK BERISLAV; MIHALJEVIC VLATKA BENCETIC; ISTUK ZORICA MARUSIC; KAPIC SAMRA; HRVACIC BOSKA; BRAJSA KARMEN; TAVCAR BRANKA; JELIC DUBRAVKO; GLOJNARIC INES; VERBANAC DONATELLA; CULIC OGNJEN; PADOVAN JASNA; ALIHODZIC SULEJMAN; HABER VESNA ERAKOVIC; SPAVENTI RADAN,期刊：Journal of Medicinal Chemistry, 页码：6111-6123 , 文章类型： Article，,卷期：2012年55-13] Macrolide antibiotics, like erythromycin, clarithromycin, and azithromycin, possess anti-inflammatory properties. These properties are considered fundamental to the efficacy of these three macrolides in the treatment of ... Selective Mode of Action of Guanidine-Containing Non-Peptides at Human NPFF Receptors [作者：FINDEISEN MARIA; WUERKER CAECILIA; RATHMANN DANIEL; MEIER RENE; MEILER JENS; OLSSON ROGER; BECKSICKINGER ANNETTE G,期刊：Journal of Medicinal Chemistry, 页码：6124-6136 , 文章类型： Article，,卷期：2012年55-13] The binding pocket of both NPFF receptors was investigated, focusing on subtype-selective behavior. By use of four nonpeptidic compounds and the peptide mimetics RF9 and BIBP3226, agonistic and antagonistic properties we... Discovery of a Novel Glucagon Receptor Antagonist N-[(4-{(1S)-1-[3-(3, 5-Dichlorophenyl)-5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phe nyl)carbonyl]-beta-alanine (MK-0893) for the Treatment of Type II Diabetes [作者：XIONG YUSHENG; GUO JIAN; CANDELORE MARI R; LIANG RUI; MILLER COREY; DALLASYANG QING; JIANG GUOQIANG; MCCANN PEGGY E; QURESHI SAJJAD A; TONG XINCHUN; XU SHIYAO SHERRIE; SHANG JACKIE; VINCENT STELLA H; TOTA LAURIE M; WRIGHT MICHAEL J; YANG XIAODONG; ZHANG BEI B; TATA JAMES R; PARMEE EMMA R,期刊：Journal of Medicinal Chemistry, 页码：6137-6148 , 文章类型： Article，,卷期：2012年55-13] A potent, selective glucagon receptor antagonist 9m, N-[(4-{(1S)-1-[3-(3,5-dichlorophenyl) -5-(6-methoxynaphthalen-2-yl)-1H-pyrazol-1-yl]ethyl}phenyl)-carbonyl]-beta-alanine, was discovered by optimization of a previousl... Structure-Based Design of Potent Bcl-2/Bcl-xL Inhibitors with Strong in Vivo Antitumor Activity [作者：ZHOU HAIBIN; AGUILAR ANGELO; CHEN JIANFANG; BAI LONGCHUAN; LIU LIU; MEAGHER JENNIFER L; YANG CHAOYIE; MCEACHERN DONNA; CONG XIN; STUCKEY JEANNE A; WANG SHAOMENG,期刊：Journal of Medicinal Chemistry, 页码：6149-6161 , 文章类型： Article，,卷期：2012年55-13] Bcl-2 and Bcl-xL are key apoptosis regulators and attractive cancer therapeutic targets. We have designed and optimized a class of small-molecule inhibitors of Bcl-2 and Bcl-xL containing a 4,5-diphenyl-1H-pyrrole-3-carb... Diphenylpyridylethanamine (DPPE) Derivatives as Cholesteryl Ester Transfer Protein (CETP) Inhibitors [作者：HARIKRISHNAN LALGUDI S; FINLAY HEATHER J; QIAO JENNIFER X; KAMAU MUTHONI G; JIANG JI; WANG TAMMY C; LI JAMES; COOPER CHRISTOPHER B; POSS MICHAEL A; ADAM LEONARD P; TAYLOR DAVID S; CHEN ALICE YE A; YIN XIAOHONG; SLEPH PAUL G; YANG RICHARD Z; SITKOFF DOREE F; GALELLA MICHAEL A; NIRSCHL DAVID S; VAN KIRK KATY; MILLER ARTHUR V; HUANG CHRISTINE S; CHANG MING; CHEN XUEQING; SALVATI MARK E; WEXLER RUTH R; LAWRENCE R MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：6162-6175 , 文章类型： Article，,卷期：2012年55-13] A series of diphenylpyridylethanamine (DPPE) derivatives was identified exhibiting potent CETP inhibition. Replacing the labile ester functionality in the initial lead 7 generated a series of amides and ureas. Further op... Discovery and Optimization of C-2 Methyl Imidazopyrrolopyridines as Potent and Orally Bioavailable JAK1 Inhibitors with Selectivity over JAK2 [作者：ZAK MARK; MENDONCA ROHAN; BALAZS MERCEDESZ; BARRETT KATHY; BERGERON PHILIPPE; BLAIR WADE S; CHANG CHRISTINE; DESHMUKH GAURI; DEVOSS JASON; DRAGOVICH PETER S; EIGENBROT CHARLES; GHILARDI NICO; GIBBONS PAUL; GRADL STEFAN; HAMMAN CHRIS; HANAN EMILY J; HARSTAD ERIC; HEWITT PETER R; HURLEY CHRISTOPHER A; JIN TIAN; JOHNSON ADAM; JOHNSON TONY; KENNY JANE R; KOEHLER MICHAEL F T; KOHLI PAWAN BIR; KULAGOWSKI JANUSZ J; LABADIE SHARADA; LIAO JIANGPENG; LIIMATTA MARYA; LIN ZHONGHUA; LUPARDUS PATRICK J; MAXEY ROBERT J; MURRAY JEREMY M; PULK REBECCA; RODRIGUEZ MADELEINE; SAVAGE SCOTT; SHIA STEVEN; STEFFEK MICAH; UBHAYAKAR SAVITA; ULTSCH MARK; VAN ABBEMA ANNE; WARD STUART I; XIAO LING; XIAO YISONG,期刊：Journal of Medicinal Chemistry, 页码：6176-6193 , 文章类型： Article，,卷期：2012年55-13] Herein we report the discovery of the C-2 methyl substituted imidazopyrrolopyridine series and its optimization to provide potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2. The C-2 methyl substit... Synthesis, Biological Evaluation, and Structure-Activity Relationships of Novel Substituted N-Phenyl Ureidobenzenesulfonate Derivatives Blocking Cell Cycle Progression in S-Phase and Inducing DNA Double-Strand Breaks [作者：TURCOTTE VANESSA; FORTIN SEBASTIEN; VEVEY FLORENCE; COULOMBE YAN; LACROIX JACQUES; COTE MARIEFRANCE; MASSON JEANYVES; CGAUDREAULT RENE,期刊：Journal of Medicinal Chemistry, 页码：6194-6208 , 文章类型： Article，,卷期：2012年55-13] Twenty-eight new substituted N-phenyl ureido-benzenesulfonate (PUB-SO) and 18 N-phenylureidobenzene-sulfonamide (PUB-SA) derivatives were prepared. Several PUB-SOs exhibited antiproliferative activity at the micromolar l...